产品
编 号：F096451
分子式：C22H23F3N4
分子量：400.44
分子式：C22H23F3N4
分子量：400.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1254977-87-1
产品详情
生物活性：
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
体内研究：
JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog.
体外研究：
JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux.
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
体内研究：
JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog.
体外研究：
JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux.
产品资料
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